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With the recent expanse of technology to
2020-12-10
With the recent expanse of technology to evaluate synthetic lethality, new combinations with DHODH inhibitors may be uncovered (O'Neil, Bailey, & Hieter, 2017). Many oncogenic backgrounds share synthetic lethality with DHODH. Cells with mutant PTEN have increased glutamine metabolism and are sensiti
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br Conclusion New series of thiazolo d pyridazine
2020-12-10
Conclusion New series of thiazolo[4,5-d]pyridazine and imidazo[2′,1′:2,3]thiazolo[4,5-d]pyridazine were designed and synthesized using thiazole as scaffold based on its previously observed activity as DHFR inhibitor. Compounds 13 and 43 (Fig. 9) proved to be the most active DHFR inhibitors with I
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DDR upregulation in patients with kidney diseases
2020-12-10
DDR1 upregulation in patients with kidney diseases such as lupus nephritis and Goodpasture's syndrome [8] as well as in animal models of kidney injury [7], [8], [18] suggests that DDR1 plays an important role in kidney disease. Studies in various mouse models of kidney injury indicate that DDR1 dele
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Expression of DDR in endothelial cells has
2020-12-10
Expression of DDR1 in endothelial cells has been previously described in human corneal blood vessels, and more recently, in murine atherosclerotic plaques (Franco et al., 2008, Mohan et al., 2001). So far, there is a lack of evidence for DDR1 expression in endothelial cells in the mouse NVP-ADW742 m
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Introduction The term myeloproliferative disorders was first
2020-12-10
Introduction The term “myeloproliferative disorders” was first proposed by William Dameshek in 1951. With the discovery of the Philadelphia chromosome, myeloproliferative disorders were classified into two groups: BCR-ABL positive chronic myeloid leukemia (CML) and BCR-ABL negative chronic myelopro
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In summary our data show
2020-12-10
In summary, our data show a novel mechanism: CPD-mediated autoprocessing of C difficile toxins regulates their proinflammatory activities. Thus, our study provides a new understanding of the molecular mechanisms of the pathogenesis of C difficile toxins and insights into designing new therapeutics a
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In the livers mefenamic acid ibuprofen and
2020-12-10
In the livers, mefenamic acid, ibuprofen, and meloxicam significantly reduced expression of both 20-HETE and EETs synthesizing cyp450 genes (ANOVA, p value in the liver and kidney samples of NSAID treated mice compared with the control group. However, this elevation was not significantly different
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To ascertain that the slower migrating bands
2020-12-10
To ascertain that the slower migrating bands represented phosphorylated CDK5, we performed a phosphatase assay. Lysates of 1478 co-expressing p35 and either WT or D144N CDK5 were immunoprecipitated using an anti-p35 antibody. The immunoprecipitates were then dephosphorylated using SAP along with ap
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phosphocholine Leukotrienes themselves are implicated in
2020-12-10
Leukotrienes themselves are implicated in the development of gastrointestinal ulcers, asthmas, and different inflammatory processes [18], [19]. It is noteworthy that COX isozymes and LOX share the same substrate arachidonic acid; therefore, inhibition of prostaglandins production by cyclooxygenase p
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A widely accepted mechanism to differentiate hESCs into card
2020-12-09
A widely accepted mechanism to differentiate hESCs into cardiomyocytes is through perturbation of the canonical Wnt/β-catenin pathway. Initial Wnt activation is required to form the Miltefosine receptor [3]. Thereafter, it is believed that inhibition of the canonical Wnt/β-catenin pathway is pivotal
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This study focused on NPC L because it is critical
2020-12-09
This study focused on NPC1L1 because it is critical for intestinal apexbio calculator of both dietary and biliary cholesterol.1, 7, 8 Overall, regulation in the intestine of cholesterol, BAs, and lipids by FGF19 and SHP may involve the combined actions of regulation of other genes that were identif
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The ADME profile of AAT was very promising
2020-12-09
The ADME profile of AAT-008 () was very promising, with high stability in HLM. The pre-clinical pharmacokinetic properties of AAT-008 were also assessed in rats (Sprague-Dawley, male), dogs (beagle, male), and monkeys (cynomolgus, male). The experimentally determined parameters are summarized in .
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In addition to providing substantial insight into substrate
2020-12-09
In addition to providing substantial insight into substrate recognition, structural studies have revealed important details about mechanisms of glycosylation and HCF-1 cleavage [28,30,33]. Activation of the nucleotide-sugar is accomplished through interactions of the β-phosphate with the N-terminus
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ACAT may act as a dimer of dimer
2020-12-09
ACAT1 may act as a dimer of dimer [38]. Within each dimer, it may contain two identical sterol substrate sites (designated as site S), and one or two sterol activator site(s) (designated as site A). Site S preferentially binds pregnenolone (PREG); it can also bind a variety of sterols that contain 3
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br Materials and methods br Results
2020-12-09
Materials and methods Results and discussion Concluding remarks Enzymatic production of bioactive 9-cis-11-trans-conjugated linoleic CP 31398 dihydrochloride is part of a detoxification mechanism against linoleic acid which is a toxic and stress factor for many lactic bacteria such as Lacto
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